The biological effects of the cysteinyl leukotrienes (cysLTs, including LTC, LTD, and LTE) are transduced mainly by a pair of 7-transmembrane receptors, CysLT and CysLT BAY u9773 is a non-selective antagonist of the CysLT receptors, having about the same IC (20-80 nM) for the inhibition of LT responses in a variety of tissue preparations containing either/or both receptors. In contrast, many of the commercially developed CysLT receptor antagonists (pranlukast or montelukast) antagonize only CysLT receptors. BAY u9773 is thus one of the only available tools for blocking CysLT receptors.
BAY-u 9773 is a selective cysteinyl-leukotriene receptor antagonist. BAY-u 9773 competitively antagonizes cysteinyl-leukotriene-induced contractions at typical and atypical cysteinyl-leukotriene receptors with comparable activity. BAY-u 9773 can be used for the research of trichomoniasis.
体外研究
BAY u9773 (10 nM-10 μM; 15 minutes) competitively displaced [3H] leukotriene D4 binding to guinea pig lung membranes, with an average pKi of 7.0.
BAY-u 9773 (1-10 μM; 30-minute pretreatment) dose-dependently inhibited MCP-1 secretion induced by TvSP and LTC4 in HMC-1 cells, with the strongest effect observed at 10 μM.
BAY-u 9773 (1-5 μM) dose-dependently inhibited ROS production induced by TvSP and LTC4 in HMC-1 cells, with significant inhibition observed at concentrations ≥1 μM.
BAY-u 9773 (5 μM) can inhibit TvSP- and LTC4-induced HMC-1 cell migration, with an inhibition rate of approximately 60%.
BAY-u 9773 (1-5 μM) dose-dependently inhibited degranulation (detected by CD63 expression) induced by TvSP and LTC4 in HMC-1 cells, with the most potent effect at 5 μM.
BAY-u 9773 can inhibit TvSP-induced p47phox phosphorylation in HMC-1 cells.
BAY-u 9773 can inhibit NF-κB phosphorylation induced by TvSP and LTC4 in HMC-1 cells.
ELISA Assay
Cell Line:
HMC-1
Concentration:
1 μM; 3 μM; 10 μM
Incubation Time:
30 min pretreatment
Result:
Dose-dependently inhibited TvSP-induced MCP-1 secretion, reducing levels to ~260 pg/mL at 10 μM compared to ~460 pg/mL in untreated TvSP-stimulated cells.
Dose-dependently inhibited LTC4-induced MCP-1 secretion, reducing levels to ~270 pg/mL at 10 μM compared to ~460 pg/mL in untreated LTC4-stimulated cells.
体内研究
BAY-u 9773 (intravenous injection) can induce dose-dependent bronchoconstriction in anesthetized guinea pigs.